Dissolution Challenges Associated with the Surface pH of Drug Particles: Integration into Mechanistic Oral Absorption Modeling

Dissolution Challenges Associated with the Surface pH of Drug Particles: Integration into Mechanistic Oral Absorption Modeling

Publication: AAPS J
Software: GastroPlus®

The present work aimed to differentiate between in vitro dissolution profiles of ibuprofen as input for GastroPlus™ and to see the impact on systemic exposure.

Preferential Solvation Study of the Synthesized Aldose Reductase Inhibitor (SE415) in the {PEG 400 (1) + Water (2)} Cosolvent Mixture and GastroPlus-Based Prediction

Preferential Solvation Study of the Synthesized Aldose Reductase Inhibitor (SE415) in the {PEG 400 (1) + Water (2)} Cosolvent Mixture and GastroPlus-Based Prediction

Publication: ACS Omega
Software: GastroPlus®

(Z)-N-Benzyl-2-{2,4-dioxo-5-(4-prop-2-yl-1-yloxyl)benzylidene)thiazolin-3-yl)}acetamide (SE415) is a novel aldose reductase inhibitor used in the management of diabetes mellitus (DM) and associated complications.

Transition from Syringe to Autoinjector Based on Bridging Pharmacokinetics and Pharmacodynamics of the P2Y12 Receptor Antagonist Selatogrel in Healthy Subjects

Transition from Syringe to Autoinjector Based on Bridging Pharmacokinetics and Pharmacodynamics of the P2Y12 Receptor Antagonist Selatogrel in Healthy Subjects

Publication: Clinical Pharmacokinetics

Selatogrel is a potent, reversible, and selective antagonist of the platelet P2Y12 receptor currently developed for the treatment of acute myocardial infarction (AMI).

Level A IVIVC for immediate release tablets confirms in vivo predictive dissolution testing for ibuprofen

Level A IVIVC for immediate release tablets confirms in vivo predictive dissolution testing for ibuprofen

Publication: Int J Pharm

A bioequivalence study comparing two fixed dose combination tablets containing 200 mg ibuprofen and 30 mg pseudoephedrine hydrochloride showed bioequivalence for pseudoephedrine AUC and Cmax, but the reference product showed higher Cmax than the test product in fasted conditions.

Identification of phenylcarbamoylazinane-1,3,4-oxadiazole amides as lipoxygenase inhibitors with expression analysis and in silico studies

Identification of phenylcarbamoylazinane-1,3,4-oxadiazole amides as lipoxygenase inhibitors with expression analysis and in silico studies

Publication: Bioorg Chem
Software: ADMET Predictor®
Therapeutic Areas: Inflammation

In search for new anti-inflammatory agents that inhibit the enzymes of arachidonic acid pathway as the drug targets, the present article describes the screening...

A novel chemical inhibitor suppresses breast cancer cell growth and metastasis through inhibiting HPIP oncoprotein

A novel chemical inhibitor suppresses breast cancer cell growth and metastasis through inhibiting HPIP oncoprotein

Publication: Cell Death Disc
Software: ADMET Predictor®
Therapeutic Areas: Oncology

Increasing evidence suggests the pivotal role of hematopoietic pre-B-cell leukemia transcription factor (PBX)-interacting protein (HPIP/PBXIP1) in cancer development and progression...

Best practices in current models mimicking drug permeability in the gastrointestinal tract – an UNGAP review

Best practices in current models mimicking drug permeability in the gastrointestinal tract – an UNGAP review

Publication: Eur J Pharm Sci
Software: GastroPlus®

The absorption of orally administered drug products is a complex, dynamic process, dependant on a range of biopharmaceutical properties; notably the aqueous solubility of a molecule, stability within the gastrointestinal tract (GIT) and permeability.

Exposure-Response Analysis to Support Nivolumab Once Every 4 Weeks Dosing in Combination with Cabozantinib in Renal Cell Carcinoma

Exposure-Response Analysis to Support Nivolumab Once Every 4 Weeks Dosing in Combination with Cabozantinib in Renal Cell Carcinoma

Publication: Clin Cancer Res

A benefit:risk assessment for a less-frequent nivolumab 480 mg Q4W + cabozantinib 40 mg QD dosing regimen was predicted using modeling and simulation of clinical trial data from nivolumab monotherapy studies and

Using PBPK M&S to support the development of an IR tablet formulation & setting more relevant dissolution test specifications

Using PBPK M&S to support the development of an IR tablet formulation & setting more relevant dissolution test specifications

Authors: Duque MD
Software: GastroPlus®
Division: PBPK

Development of formulation and setting dissolution test specifications for IR tablets based on PBPK modeling & simulation – amiodarone as a case example

Predicting the Drug–Drug Interaction Mediated by CYP3A4 Inhibition: Method Development and Performance Evaluation

Predicting the Drug–Drug Interaction Mediated by CYP3A4 Inhibition: Method Development and Performance Evaluation

Publication: AAPS J
Software: GastroPlus®

The prediction of drug–drug interactions (DDIs) plays critical roles for the estimation of DDI risk caused by inhibition of CYP3A4.